Upgrade to enjoy subscriber-only features like email alerts and data export. See the Plans and Pricing
|Title:||Polymer conjugates of opioid antagonists|
|Abstract:||The invention provides polymer conjugates of opioid antagonists comprising a polymer, such as poly(ethylene glycol), covalently attached to an opioid antagonist. The linkage between the polymer and the opioid antagonist is preferably hydrolytically stable. The invention also includes a method of treating one or more side effects associated with the use of opioid analgesics, such as constipation, nausea, or pruritus, by administering a polymer conjugate of the invention.|
|Inventor(s):||Bentley; Michael David (Huntsville, AL), Roberts; Michael James (Williamsburg, VA), Shen; Xiaoming (Madison, AL), Cheng; Lin (Huntsville, AL)|
|Assignee:||Nektar Therapeutics (San Francisco, CA)|
|Filing Date:||Oct 06, 2009|
|Claims:||1. A pharmaceutical composition comprising a polymer conjugate; an opioid agonist; and a pharmaceutically acceptable carrier, wherein the polymer conjugate has the formula: ##STR00009## or pharmaceutically acceptable salt thereof, wherein: Y is allyl; Z is OH; X is --NHC(O)--, --NH--, --OC(O)NH--, --O--, --S-- or --NHC(O)NH--; and POLY is methoxy poly(ethylene glycol), wherein POLY has a molecular weight of from about 100 Da to about 800 Da; and wherein the pharmaceutical composition is formulated into a form suitable for oral administration. |
2. The pharmaceutical composition of claim 1, wherein the opioid agonist is selected from the group consisting of alfentanil, bremazocine, buprenorphine, butorphanol, codeine, cyclazocine, dezocine, diacetylmorphine, dihydrocodeine, fentanyl, hydrocodone, hydromorphone, levorphanol, meperidine (pethidine), methadone, morphine, nalbuphine, noscapine, oxycodone, oxymorphone, papaverine, pentazocine, pethidine, phenazocine, propiram, propoxyphene, sufentanil, thebaine and tramadol.
3. The pharmaceutical composition of claim 1, wherein POLY has a molecular weight of from about 100 Da to about 500 Da.
4. The pharmaceutical composition of claim 1, wherein X is --O--.
Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.